Table 1. Summary of published case reports on selective androgen receptor modulators (SARMs)-induced liver injury.
*Converted value.
Reference ranges are included in parenthesis wherever available; all parameters are in SI units.
Bi: bilirubin; ALT: alanine aminotransferase; AST: aspartate aminotransferase; ALP: alkaline phosphatase; GGT: gamma-glutamyl transferase; PC: platelet count; INR: international normalized ratio; NR: not reported
| Author | Age and Sex | Presentation | Agent (duration) | Alcohol use | Bilirubin (Bi) presentation > Bi peak | ALT presentation > ALT peak | AST presentation > AST peak | ALP presentation > ALP peak | GGT on presentation | PC on presentation | INR on presentation | R-ratio | RUCAM score | Imaging | Histology | Treatment | Prognosis |
| Flores et al. in 2020 [19] | 24-year-old male | Jaundice, anorexia, nausea, lethargy, 5 kg weight loss for 5 weeks; 1 week after cessation of agent | Ligandrol (9 weeks) | Binge drinking once a month | 116 µmol/L (2-20) > 116 µmol/L at week 0 | 4.53 µkat/L*(<0.66*) > 9.78 at 2 weeks | 1.84 µkat/L*(<0.66*) > 2.91 µkat/L* at 2 weeks | 4.82 µkat/L* (0.5-1.83*) > 4.82 µkat/L* | 1.03 µkat/L*(<1.83) | 387 x 109 (150-450) | 1.0 | 8.22 | 7 | Liver US - no biliary obstruction | NR | NR | 4 months for enzymes to return to baseline |
| Flores et al. in 2020 [19] | 49-year-old male | Jaundice and itching for 5 weeks | RAD-140 (intermittently for 4 weeks, 4 months) | Insignificant | 291 µmol/L (2-20) > 346 µmol/L at 3 weeks, | 0.86 µkat/L*(<0.66*) > 2.86 µkat/L* at 8 weeks | 0.98 µkat/L*(<0.66*) > 2.04 µkat/L* at 8 weeks | 5.45 µkat/L*(0.5-1.83*) > 5.45 µkat/L* at week 0 | NR | 347 x 109 (150-450 x 109) | 1.2 | 5.0 | 6 | Liver imaging - no biliary obstruction | Moderate cholestasis with ductopenia and minimal fibrosis and inflammation | Ursodiol, cholestyramine | 12 months for enzymes to return to baseline |
| Barbara et al. in 2020 [20] | 32-year-old-male | Fatigue, pruritus, and weight loss for 50 days | Ligandrol 10 mg daily (2 weeks) | NR | 41 µmol/L* > 653.22 µmol/L*at Day 46 | 3.8 µkat/L* > 4.05 µkat/L* on day 26 | 91 IU/L > 1.51 µkat/L* on day 22 | .47 µkat/L*>0.75 µkat/L* at day 54 | NR | NR | 1.1 | NR | NR | Abdominal US and CT - hepatomegaly; MRCP - small hepatic cyst, splenomegaly, no biliary dilatation | Cholestatic hepatitis with mild portal, periportal, and perisinusoidal fibrosis; no hyaline globules on PAS diastase stain, 2+ irons staining of hepatocytes | NR | NR |
| Koller et al. in 2021 [21] | 19-year-old-male | Dark urine, yellow sclera, thin light-colored stools, after 3 weeks of PCT | Ligandrol once capsule daily (4 weeks, 3 weeks of post-cycle therapy) | None | 238 µmol/L (3.4-17.1) > NR | ALT 2.2 µkat/L (0.2-0.80) > NR | NR | ALP 1.54 µkat/L (0.67-2.15) > NR | 0.41 µkat/L (0.18- 1.02) | NR | NR | 3.9 | 6 | Abdominal US - normal liver and spleen size, no duct dilation | Mild septal fibrosis, and canalicular cholestasis in the hepatocytes with numerous biliary plugs. Few necrotic hepatocytes, centrilobular mostly lymphocytic infiltrate, and ductopenia. | 1000 mg ursodiol daily for 2 months | 3 months for enzymes to return to baseline |
| Koller et al. in 2021 [21] | 28-year-old-male | Nausea, fatigue, and jaundice, after 4th dose of PCT | Ligandrol (3 months), and Ostarine (3 weeks later ) | None | 401 µmol/L > NR | 2.4 µkat/L > NR | NR | 1.54 µkat/L > NR | NR | NR | NR | 3.3 | NR | MRI - hepatomegaly without biliary pathology | Mild bridging fibrosis, destruction of bile ducts, centrilobular canalicular cholestasis with numerous bile plugs in the canaliculi, phagocytosis hepatocellular apoptosis, and perivenular necrosis | 300 mg intravenous N-acetyl cysteine 4 times daily, 1000 mg oral ursodiol daily, and 450 mg silymarin daily | NR |
| Bedi et al. in 2021 [22] | Early 40s male | Jaundice, anorexia, weight loss, lethargy, diarrhea | Ostarine (2 months) | None | 0.34 µmol/L > 0.735 µmol/L at 4 weeks | 1.86 µkat/L* > NR | 1.15 µkat/L* > NR | 268 U/L > NR | 49 U/L | 313x 109 | 1.3 | 0.8 | NR | US and CT - negative for duct dilatation, cirrhosis, hepatomegaly, and intraabdominal VTE; MRCP - normal hepatic and biliary anatomy | Mild bile ductular reaction with very mild duct damage and minimal inflammation; moderate to severe cholestasis | NR | Gradual improvement over several months |
| This study | 20-year-old-male | Dark urine, light stools, pruritus | RAD-140 (4 months) | None | 427.5 µmol/L* (5.13-20.52) > 533.5 µmol/L* at 7 days | 1.66 µkat/L* (0-0.56*) > 2.56 µkat/L* at 28 days | 1.18 µkat/*L (0-0.56*) > 1.69 µkat/L* at 28 days | 5.38 µkat/L* (0.73-2*) > 7 µkat/L* at 14 days | NR | NR | 0.9 | 1.5 | 4 | US-biliary sludge; MRCP - mild segmental narrowing involving intrahepatic ducts; ERCP-normal cholangiogram, no signs of PSC, no strictures/narrowing | Mixed portal hepatitis, cholestasis, and biliary reactive changes, numerous ceroid-laden macrophages | Supportive measures | Bi improved from 530 to 188 at 4 weeks after follow-up, clinical progression is still being monitored. |